KN-93,139298-40-1

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抑制剂描述：

产品名称：KN-93

产品别名：见爱必信官网

英文别名：KN-93

靶点：CaMK

CAS：139298-40-1

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：

KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).

溶解性：DMSO > 10mM

体外研究：

After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, epidermal growth factor, and insulin-like growth factor-1 in NIH 3T3 fibroblasts. KN-93 inhibits the H+, K+-ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca2+-independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93. KN-93 (10 μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells.

体内研究：KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes, and suppresses phosphorylation of CaMKII and NF-κB in diabetic retina.

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